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Short Paper | Regular issue | Vol 106, No. 4, 2023, pp.742-757
Published online, 10th March, 2023
DOI: 10.3987/COM-23-14824
Synthesis and Biological Evaluation of 5-Methylpyrimidine Derivatives as Dual Inhibitors of EGFR and Src for Cancer Treatment

Yaqing Zuo, Kehui Chen, Ying Xu, Yi Le, and Longjia Yan*

*School of Pharmaceutical Sciences, Guizhou University, Guiyang 550025, China


In this paper, a series of new 5-methylpyrimidine derivatives was designed as dual inhibitors of EGFR and Src for cancer treatment. Twenty new compounds were synthesized and evaluated for antitumor activity with A549, HepG2, and K562 cells. Compounds 8f, 8p, and 8q showed better antitumor activity than Gefitinib and Dasatinib. They were selected for testing inhibition of EGFR and Src. The IC50 values of the most potent compound 8p was reached to 1.56 μM and 0.74 μM. In addition, the ADMET properties of compounds 8f, 8o-8q were predicted with ADMETlab 2.0.